Biochem/physiol Actions

Target IC₅₀: 41 nM against Syk; 460 nM against FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro

Primary TargetSyk

Reversible: yes

Product competes with ATP.

Cell permeable: yes

General description

A cell-permeable pyrimidine-carboxamide compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Syk (IC₅₀ = 41 nM), while affecting PKC_ε, PKC_βII, ZAP-70, Btk, and Itk only at much higher concentrations (IC₅₀ = 5.1, 11, 11.2, 15.5, and 22.6 µM, respectively). Inhibits FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC₅₀ = 460 nM) and passive cutaneous anaphylaxis (PCA) reaction in mice in vivo (ID₅₀ = 13.2 mg/kg, s.c.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Hisamichi, H., et al. 2005. Bioorg. Med. Chem.13, 4936.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Irritant (B)